1. Field of the Invention
The subject invention generally relates to a gastroretentive composition. More specifically, the subject invention relates to a gastroretentive composition that includes an excipient component and an active ingredient component. The gastroretentive composition is used as a floating drug delivery system (FDDS).
2. Description of the Related Art
Medicinal compositions are typically administered in doses to a body to cure, minimize, and/or prevent symptoms of illness and/or injury. A medicinal composition may be administered in many different ways. For example, a medicinal composition may be administered orally as a liquid or tablet to absorb through a stomach, by inhalation as a vapor into a lung, or by injection as a liquid into a vein or a muscle. Oral administration of medicinal compositions is most typical due to ease of administration and increased likelihood of patient compliance.
Medicinal compositions may be useful for immediate or extended- and/or sustained-release in the body. Immediate-release compositions deliver a complete dose upon administration. In contrast, extended- and/or sustained-release compositions enable prolonged and continuous input of the dose to the body. Extended- and/or sustained-release compositions may be further classified according to function. For example, a gastroretentive composition is an extended- and/or sustained-release composition that remains in the stomach for an extended residence time to allow spatial- and time-controlled dose delivery. Gastroretentive compositions are typically selected for applications which require improved solubility in a low pH environment such as the stomach.
Gastroretentive compositions may be used as floating drug delivery systems where the gastroretentive composition floats aloft gastric fluids in the stomach. Floating drug delivery systems are less likely to be expelled from the stomach prematurely as compared to other extended- and/or sustained-release compositions since solids are typically expelled from the stomach before gastric fluids.
Gastroretentive compositions may be produced by wet granulation or dry granulation, and typically comprise an active ingredient and at least one excipient, such as a binder, a coating, a filler, or a lubricant. Wet granulation is conducted by adding a liquid binder to the active ingredient to produce a wet granulate, screening the wet granulate into pellets, drying and adding a dry lubricant to the pellets, and compressing the pellets in a die to form tablets. In contrast, dry granulation is conducted on a press or a roller compactor using only dry active ingredients and excipients. Dry granulation is useful for active ingredients that are sensitive to moisture, and is typically selected for applications that require shorter processing times, streamlined equipment, and decreased equipment and raw material costs.
Many existing gastroretentive compositions include excipients comprising gas-generating ingredients such as inorganic bases and organic acids. Such gas-generating ingredients react with ambient moisture and contribute to instability and premature dissolution of the gastroretentive compositions during storage.
Additionally, many existing gastroretentive compositions have higher bulk densities than gastric fluids. Higher bulk densities prevent flotation aloft gastric fluids. Without flotation aloft gastric fluids, the gastroretentive compositions are prematurely expelled from the stomach without adequate residence time for absorption into the body.
Further, many existing gastroretentive compositions are prone to moisture absorption. Moisture absorption may decrease an effectiveness of active ingredients, alter a chemical composition of active ingredients, and/or contribute to instability and premature dissolution of gastroretentive compositions during storage and/or administration.
Finally, many existing gastroretentive compositions exhibit low binding properties. Low binding properties require gastroretentive compositions to be produced by wet granulation, which increases processing times and equipment and raw material costs as compared to dry granulation.
Due to the inadequacies of the existing gastroretentive compositions, there remains an opportunity to provide a gastroretentive composition which improves upon existing gastroretentive compositions.